CN101897925B - Medicinal composition for treating metabolic syndrome - Google Patents

Medicinal composition for treating metabolic syndrome Download PDF

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Publication number
CN101897925B
CN101897925B CN200910263426.5A CN200910263426A CN101897925B CN 101897925 B CN101897925 B CN 101897925B CN 200910263426 A CN200910263426 A CN 200910263426A CN 101897925 B CN101897925 B CN 101897925B
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rhizoma coptidis
component
rhizoma
effective ingredient
curcumae longae
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CN200910263426.5A
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CN101897925A (en
Inventor
杨奎
张怀莉
柯玥珺
邬春久
刘如练
陈科
张明洪
毛旭华
马宣毅
李亚丽
向靓
黄薇
闵志强
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CHENGDU BAIKANG MEDICINE INDUSTRIAL PHARMACOLOGY AND TOXICOLOGY RESEARCH INSTITUTE
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CHENGDU BAIKANG MEDICINE INDUSTRIAL PHARMACOLOGY AND TOXICOLOGY RESEARCH INSTITUTE
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Abstract

The invention relates to a medicinal composition preparation of golden thread and turmeric, a medicinal composition preparation of active ingredients or components of the golden thread and active ingredients or components of the turmeric, a medicinal composition preparation of the golden thread and the active ingredients or components of the turmeric, and a medicinal combined preparation of the turmeric and the active ingredients or components of the golden thread. The preparations can be used for treating the metabolic syndrome. The invention also relates to a method for preparing the medicinal composition preparations and use of the medicinal composition preparations in the treatment of metabolic syndrome.

Description

A kind of pharmaceutical composition for the treatment of metabolic syndrome
Invention field
The present invention relates to the medicine composition of the medicine composition of Rhizoma Coptidis and Rhizoma Curcumae Longae, the medicine composition of Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component, the medicine composition of Rhizoma Coptidis and turmeric effective ingredient or component, Rhizoma Curcumae Longae and Rhizoma Coptidis effective ingredient or component.This kind of preparation can be used for treating metabolic syndrome.The invention still further relates to preparation method and the purposes of this kind of medicine composition in treatment of metabolic of this kind of medicine composition.
Background of invention
Reaven in 1988 notices that dyslipidemias, hypertension, hypertriglyceridemia often pool together, and proposes the concept of " X-syndrome, X-Syndrome ", and using the main feature of insulin resistance as X syndrome.In view of this syndrome and multiple metabolism related diseases have close contacting, Zimmet in 1997 etc. advocate its called after metabolic syndrome.Metabolic syndrome (metabolicsyndrome, MS) be the pathological state of multiple Metabolite abnormal aggregation, comprise: 1. abdominal obesity or overweight, 2. (high triglyceride (TG) mass formed by blood stasis and HDL-C (HDL-C) are low, 3. hypertension and 4. insulin resistance and/or impaired glucose tolerance for atherogenicity dyslipidemia.Microalbuminuria, hyperuricemia is also comprised and short inflammatory conditions (C reactive protein CRP) increases and short thrombosis state (Fibrinogen increases and Fibrinolytic activity-1, PAI-1) increases in some standard.The gathering of these compositions appears in same individuality, and the risk of trouble cardiovascular disease is greatly increased.
Due to the risk factor that each composition in metabolic syndrome is all cardiovascular diseases, their synergy is stronger, so there is people metabolic syndrome to be called " dead quartet " (central obesity, hyperglycemia, hypertriglyceridemia and hypertension), therefore metabolic syndrome is the total concept to the generality of one group of height correlation disease and the Clinics and Practices of economy, require carry out life style intervention (as lose weight, increase physical training and spirit coordinate), blood sugar lowering, adjust fat and antihypertensive therapy all of equal importance.All treatments all should around the various risk factor of reduction.Comprise and effectively losing weight; Alleviate insulin resistant; Good control blood glucose; Improve disorders of lipid metabolism, control blood pressure etc.
It is dirty that Chinese medical discrimination thinks that metabolic syndrome relates to liver,spleen,kidney three, and in its evolution in early days based on the imbalance of internal organs negative and positive of qi and blood, mid-term is become heavily with phlegm-damp mutually, and stage cold and heat, deficiency and excess, the stasis of blood are turbid interlocks and shows for fruit.Wherein, scorchingly in the morbidity of metabolic syndrome, pivotal role is played.All think that the main pathogenesis of quenching one's thirst is scorching impairment of YIN at all times." Plain Questions lose consciousness opinion ": " the large intestine transfering pathogenic heat to the stomach, polyphagia but emaciation people ", " Ling Shu Miraculous Pivot or Divine Axis is a disciple of ": " pathogenic heat in the stomach; then rapid digestion of food, make us county's favourable signs of the heart hungry ", " the deficient dysuria stranguria of quenching one's thirst of gold " cloud: " FU YANG pulse being floating and rapid is floated as gas; number is the large heavily fortified point of rapid digestion of food; excessive QI causing frequent urination, frequency of micturition and hard, and hard number is fought mutually; be and quench one's thirst ", " Medicine Comprehended three disappears " also goes: " three cards disappeared, all scorching knot poly-also ", and each physicians from a family for generations family all indicates diabetes and scorching closely related.Blood glucose person this be essence of water and grain in blood, Metabolism of Normal is then " change and red be blood ".If not normal alienation, " abnormal ascent-descent between clear YANG and turbid YIN ", raw turbid in blood system, and turbid very easily heat-transformation in blood, disturb internal organs in pathogenic heat, function is not normal, makes kidney not Gu Zang, or liver loses defeated letting out, and store blood is unfavorable, makes blood glucose raise eventually.These are all pointed out scorchingly has substantial connection with metabolism of blood glucose.Metabolic syndrome patients is all fatter, " fertile people's excessive phlegm wets ", and main pathogenesis is retention of damp-heat in the interior, and the matter of wet Sheng is this, and damp-stagnancy heat-transformation is mark.Disease is sent out in wet, strongly fragrant heat-transformation of a specified duration; Vegetarian diet delicious food, damp and hot interior life; Inside and outside combined pathogens, damp and hot friendship resistance; Retention of damp-heat in the interior, dysfunction of the spleen in transportation; Insufficiency of the spleen mistake fortune, damp and hot interior life.Therapeutic principle of traditional Chinese medicine is when damp and hot based on Qinghua, and wet clearly then all diseases of reducing phlegm and internal heat all are removed.
Rhizoma Coptidis is the dry rhizome of the Rhizoma Coptidis (Copti chinensis Franch) of Ranunculaceae (Ranunculaceae), Coptis deltoidea C.Y.Cheng et Hsiao (Coptisdeltoidea C.Y.Cheng et Hsiao) or Coptis Teeta Wall (Coptis teeta Wall).Compendium of Material Medica cloud: " its root yellow skin like a chain of pearls or a string of beads, therefore named ", also known as Wang Lian, Zhi Lian, chicken feet Rhizoma Coptidis.The medicinal beginning of Rhizoma Coptidis is loaded in Shennong's Herbal, and medical material is called successively " taste connects ", " refined company ", " Coptis Teeta Wall ".Modern study shows, the effective ingredient of Rhizoma Coptidis is mainly berberine (Berberine), and have another name called berberine, content reaches about 10%, exists with hydrochloride form.The relieving restlessness of Rhizoma Coptidis effect clearing away heat and eliminating dampness, modern study confirms that Rhizoma Coptidis and effective ingredient berberine (berberine) or active component alkaloid thereof have blood sugar lowering, blood fat reducing, treatment diabetes and metabolic syndrome effect.
Rhizoma Curcumae Longae, another name Dioscorea zingiberensis, hair Rhizoma Curcumae Longae, tripod perfume, Radix Curcuma are the rhizome of zingiberaceous plant Rhizoma Curcumae Longae Curcuma longa L., the circulation of qi promoting of function removing blood stasis, inducing menstruation to relieve menalgia.Modern study shows Rhizoma Curcumae Longae and effective ingredient curcumin or Rhizoma Curcumae Longae total flavones, experimental atherosclerosis rats and rabbit are had to the effect of significantly falling total plasma cholesterol and beta lipoprotein, and can liver cholesterol be reduced, correction α-out of proportion with beta lipoprotein, but on endogenous cholesterol without impact; More remarkable to the effect of falling plasma triglyceride, triglyceride in blood plasma can be made to be reduced to below normal level.Rhizoma Curcumae Longae and effective ingredient curcumin or Rhizoma Curcumae Longae total flavones all can resist the serum lipids in rats that effect of high sucrose food causes, reduce liver heavy, reduce triglyceride, free fatty, content of phospholipid in liver, reduce the total triglyceride of serum, VLDL+LDL triglyceride, the content of HDL triglyceride, VLDL+LDL cholesterol and blood free fatty acid, improve serum total cholesterol and HDL cholesterol level, suppress the synthesis of fatty acid.Report Rhizoma Curcumae Longae and effective ingredient curcumin or Rhizoma Curcumae Longae total flavones is had to have certain therapeutical effect to metabolic syndrome in the recent period.
Because metabolic syndrome is brought out by many factors, current drug combination embodies greater advantage.We show that the medicine composition of Rhizoma Coptidis or its effective ingredient or component and Rhizoma Curcumae Longae or its effective ingredient or component exists obvious synergistic function in treatment of metabolic at research.
For being used alone Rhizoma Coptidis or its effective ingredient or component, or when being used alone Rhizoma Curcumae Longae or its effective ingredient or component, metabolic syndrome controls not good patient, the Rhizoma Coptidis of therapeutic dose and the medicine composition of Rhizoma Curcumae Longae can be provided by same unit dosage preparation in the mode of similar commercially available each stand-alone product, the medicine composition of Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component, the medicine composition of Rhizoma Coptidis and turmeric effective ingredient or component, the chemistry of the medicine composition of Rhizoma Curcumae Longae and Rhizoma Coptidis effective ingredient or component and the dosage form of physically stable are extremely of value to and control it and occur and develop in clinical metabolic syndrome is treated.
Summary of the invention
The present invention relates to for Rhizoma Coptidis and Rhizoma Curcumae Longae, Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component, Rhizoma Coptidis and turmeric effective ingredient or component, Rhizoma Curcumae Longae and Rhizoma Coptidis effective ingredient or component combine the unit dose formulations of sending, this kind of preparation can be used for treating metabolic syndrome.The invention still further relates to preparation method and the purposes of this kind of combination formulations in treatment of metabolic of this kind of unit of association dosage particles.
Technical scheme one of the present invention is: Rhizoma Coptidis 1 ~ 50g, Rhizoma Curcumae Longae 1 ~ 60g (daily dose); Above-mentioned side's medicine, takes distinct methods to extract, and obtains extract, makes the different preparations differed from one another with this extract; Extracting method (1), separately or merge, with 3-10 times of water gaging, heating decocts or reflux, extract, 2-5 time, each extraction 1-3 hour, extracting liquid filtering, and concentrating under reduced pressure, obtains extractum, for subsequent use for Rhizoma Coptidis and Rhizoma Curcumae Longae; Extracting method (2), Rhizoma Coptidis and Rhizoma Curcumae Longae separately or merge, by 3-10 times amount ethanol, heating and refluxing extraction 2-5 time, are extracted 1-3 hour, extracting liquid filtering, decompression recycling ethanol at every turn, concentrate, obtain extractum, for subsequent use.In embodiments, the present invention relates to unit dosage forms pharmaceutical composition, comprise the Rhizoma Curcumae Longae be combined with Rhizoma Coptidis, and the two extract; With choose any one kind of them or multiple pharmaceutically acceptable excipient; Be prepared into oral liquid, capsule, granule, soft gelatin capsule, tablet, dispersible tablet, oral cavity disintegration tablet, drop pill, sustained-release preparation.
Another technical scheme of the present invention is: Rhizoma Coptidis effective ingredient (berberine) or component (alkaloid) 0.005 ~ 1.0g, turmeric effective ingredient (curcumin) or component (Rhizoma Curcumae Longae total flavones) 0.05 ~ 5g (daily dose); In embodiments, the present invention relates to unit dosage forms pharmaceutical composition, comprise the turmeric effective ingredient (curcumin) or component (Rhizoma Curcumae Longae total flavones) that combine with Rhizoma Coptidis effective ingredient (berberine) or component (alkaloid); With choose any one kind of them or multiple pharmaceutically acceptable excipient; Be prepared into oral liquid, capsule, granule, soft gelatin capsule, tablet, dispersible tablet, oral cavity disintegration tablet, drop pill, sustained-release preparation.
Another technical scheme of the present invention is: Rhizoma Coptidis 1 ~ 50g, turmeric effective ingredient (curcumin) or component (Rhizoma Curcumae Longae total flavones) 0.05 ~ 5g weight portion (daily dose); In embodiments, the present invention relates to unit dosage forms pharmaceutical composition, comprise the turmeric effective ingredient (curcumin) or component (Rhizoma Curcumae Longae total flavones) that are combined with Rhizoma Coptidis; With choose any one kind of them or multiple pharmaceutically acceptable excipient; Be prepared into oral liquid, capsule, granule, soft gelatin capsule, tablet, dispersible tablet, oral cavity disintegration tablet, drop pill, sustained-release preparation.
Another technical scheme of the present invention is: Rhizoma Curcumae Longae 1 ~ 60g, Rhizoma Coptidis effective ingredient (berberine) or component (alkaloid) 0.01 ~ 1g (daily dose); In embodiments, the present invention relates to unit dosage forms pharmaceutical composition, comprise the Rhizoma Coptidis effective ingredient (berberine) or component (alkaloid) that are combined with Rhizoma Curcumae Longae; With choose any one kind of them or multiple pharmaceutically acceptable excipient; Be prepared into oral liquid, capsule, granule, soft gelatin capsule, tablet, dispersible tablet, oral cavity disintegration tablet, drop pill, sustained-release preparation.
Rhizoma Coptidis of the present invention and Rhizoma Curcumae Longae, Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component, Rhizoma Coptidis and turmeric effective ingredient or component, Rhizoma Curcumae Longae and Rhizoma Coptidis effective ingredient or component combine the unit dose formulations of sending through laboratory observation, to metabolic syndrome, there is better healing effect.The conjunctive use of Rhizoma Coptidis and Rhizoma Curcumae Longae, Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component, Rhizoma Coptidis and turmeric effective ingredient or component, Rhizoma Curcumae Longae and Rhizoma Coptidis effective ingredient or component, can Synergistic and/or complementation.
(1) the present invention's research that experimental metabolic syndrome is affected
10% fructose water fed rat after 6 weeks, detected blood triglyceride and fasting glucose (FPG), fasting insulin concentration, calculated insulin sensitivity index.Then gavage gives the present invention and combines the unit dose system of sending, and successive administration, after 6 weeks, detects blood pressure, oral glucose tolerance, glucose infusion rate, triglyceride, T-CHOL, Low-density lipoprotein and High-density lipoprotein.Table 1 ~ 4 result display, metabolic syndrome model group rats systolic pressure, fasting glucose, triglyceride, T-CHOL and High-density lipoprotein significance raise (p < 0.01), and glucose tolerance and glucose infusion rate obviously or significantly reduce (p < 0.05 ~ p < 0.01).After combined pharmaceutical formulation treatment of the present invention, metabolic syndrome rat model body weight, systolic pressure, fasting glucose, triglyceride, T-CHOL and High-density lipoprotein can be made significantly to reduce (p < 0.01), glucose tolerance and glucose infusion rate significantly raise (p < 0.01), and compare effect better (p > 0.05) with alone.
Table 1 is on the impact (x ± s) of experimental metabolic syndrome rat model blood pressure, glucose infusion rate
Table 2 is on the impact (x ± s) of experimental metabolic syndrome rat model glucose tolerance
The experimental metabolic syndrome rat model of table 3 is on the impact (g, x ± s) of rat body weight
Table 4 is on the lipometabolic impact of experimental metabolic syndrome rat model (mmol/L, x ± s)
(4) Clinical efficacy of metabolic syndrome is treated
With reference to 2002 u.s. national cholesterol education program adult treatment guide III (NCEP-ATPIII) diagnostic criteria: abdominal obesity; Waistline: male > 102cm, women > 88cm, triglyceride (TG) >=1.69mmol/L, and/or highdensity lipoprotein-cholesterol (HDL-C) reduces; Blood pressure >=130/85mmHg.Meeting above more than 3 or 3 is diagnosable metabolic syndrome.Keeping on a diet, giving up smoking, increasing on the basis such as physical sport and fat-reducing, use combined pharmaceutical formulation of the present invention and alone preparation respectively, treat 3 months.Table 5 result shows, Rhizoma Coptidis and Rhizoma Curcumae Longae combined pharmaceutical formulation and Rhizoma Coptidis alkaloid and Rhizoma Curcumae Longae total flavones combined pharmaceutical formulation treatment metabolic syndrome patients 3 months, significantly can reduce TG and fasting glucose (p < 0.01), raise HDL-C (p < 0.01), obviously than alone group better (p < 0.05).
The Clinical efficacy (mmol/L, x ± s) of metabolic syndrome treated by table 5

Claims (5)

1. combine the application in the medicine of preparation treatment metabolic syndrome of the unit dose combination formulations sent, wherein, the described unit dose combination formulations sent of combining is made up of the following component of effective dose and pharmaceutically acceptable excipient:
Rhizoma Coptidis extractum and turmeric paste, adopt and prepare with the following method: separately or merge, with 3-10 times of water gaging, heating decocts or reflux, extract, 2-5 time, each extraction 1-3 hour, extracting liquid filtering, and concentrating under reduced pressure, obtains extractum, for subsequent use for (1) Rhizoma Coptidis and Rhizoma Curcumae Longae; (2) Rhizoma Coptidis and Rhizoma Curcumae Longae are separately or merge, and by 3-10 times amount ethanol, heating and refluxing extraction 2-5 time, extract 1-3 hour, extracting liquid filtering, decompression recycling ethanol at every turn, concentrate, obtain extractum, for subsequent use; Or Rhizoma Coptidis effective ingredient or component and turmeric effective ingredient or component,
Described Rhizoma Coptidis effective ingredient or component are berberine or Rhizoma Coptidis alkaloid, and described turmeric effective ingredient or component are curcumin or Rhizoma Curcumae Longae total flavones.
2. application according to claim 1, is characterized in that, described Rhizoma Coptidis is Rhizoma Coptidis or Rhizoma Coptidis decoction pieces, and described Rhizoma Curcumae Longae is Rhizoma Curcumae Longae medical material or Rhizoma Curcumae Longae decoction pieces.
3. the application according to any one of claim 1-2, is characterized in that, Rhizoma Coptidis 1 ~ 50g, Rhizoma Curcumae Longae 1 ~ 60g.
4. application according to claim 1, wherein said combine the unit dose combination formulations sent it comprises: Rhizoma Coptidis effective ingredient or component 0.005 ~ 1.0g, turmeric effective ingredient or component 0.05 ~ 5g.
5. application according to claim 1, is characterized in that, describedly combines the unit dose combination formulations sent and chooses any one kind of them or multiple pharmaceutically acceptable excipient, is prepared into oral liquid, capsule, granule, soft gelatin capsule, tablet, drop pill, sustained-release preparation.
CN200910263426.5A 2009-12-16 2009-12-16 Medicinal composition for treating metabolic syndrome Expired - Fee Related CN101897925B (en)

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CN103479635A (en) * 2013-08-01 2014-01-01 中国人民解放军第三〇二医院 Pharmaceutical composition used for preventing and treating non-alcoholic fatty liver disease and application thereof
CN105796674B (en) * 2014-12-31 2020-08-07 上海中医药大学 Traditional Chinese medicine composition for preventing and treating metabolic syndrome
WO2018107687A1 (en) 2016-12-15 2018-06-21 深圳瑞健生命科学研究院有限公司 Method for preventing and treating hyperlipidemia
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